CA2653076A1 - Pyrazolo [1, 5-a] pyrimidines as cdk inhibitors - Google Patents

Pyrazolo [1, 5-a] pyrimidines as cdk inhibitors Download PDF

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Publication number
CA2653076A1
CA2653076A1 CA002653076A CA2653076A CA2653076A1 CA 2653076 A1 CA2653076 A1 CA 2653076A1 CA 002653076 A CA002653076 A CA 002653076A CA 2653076 A CA2653076 A CA 2653076A CA 2653076 A1 CA2653076 A1 CA 2653076A1
Authority
CA
Canada
Prior art keywords
alkyl
compound
group
aryl
heteroaryl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA002653076A
Other languages
English (en)
French (fr)
Inventor
Timothy J. Guzi
Ronald J. Doll
Amin A. Nomeir
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2653076A1 publication Critical patent/CA2653076A1/en
Abandoned legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA002653076A 2006-05-22 2007-05-21 Pyrazolo [1, 5-a] pyrimidines as cdk inhibitors Abandoned CA2653076A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US80257706P 2006-05-22 2006-05-22
US60/802,577 2006-05-22
PCT/US2007/011991 WO2007139732A1 (en) 2006-05-22 2007-05-21 Pyrazolo [1, 5-a] pyrimidines as cdk inhibitors

Publications (1)

Publication Number Publication Date
CA2653076A1 true CA2653076A1 (en) 2007-12-06

Family

ID=38544151

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002653076A Abandoned CA2653076A1 (en) 2006-05-22 2007-05-21 Pyrazolo [1, 5-a] pyrimidines as cdk inhibitors

Country Status (18)

Country Link
US (1) US20070275963A1 (de)
EP (1) EP2027127A1 (de)
JP (1) JP2009538304A (de)
KR (1) KR20090019796A (de)
CN (1) CN101495481A (de)
AR (1) AR061072A1 (de)
AU (1) AU2007268083A1 (de)
BR (1) BRPI0712016A2 (de)
CA (1) CA2653076A1 (de)
EC (1) ECSP088906A (de)
IL (1) IL195238A0 (de)
MX (1) MX2008014824A (de)
NO (1) NO20085331L (de)
PE (1) PE20080071A1 (de)
RU (1) RU2008150419A (de)
TW (1) TW200817404A (de)
WO (1) WO2007139732A1 (de)
ZA (1) ZA200809796B (de)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101903396A (zh) * 2007-11-07 2010-12-01 先灵公司 新的细胞周期关卡调节剂和它们与关卡激酶抑制剂的联合应用
BR112012005550A2 (pt) * 2009-09-11 2015-09-08 Cylene Pharmaceuticals Inc lactamas heterociclo-substituídas farmaceuticamente úteis
AU2010343102B2 (en) 2009-12-29 2016-03-24 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
MX2013012233A (es) * 2011-04-19 2014-01-23 Bayer Pharma AG 4-aril-n-fenil-1,3,5-triazin-2-aminas sustituidas.
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
WO2013059634A1 (en) 2011-10-20 2013-04-25 The Regents Of The University Of California Use of cdk9 inhibitors to reduce cartilage degradation
AU2012340200B2 (en) 2011-11-17 2017-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-Terminal Kinase (JNK)
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
HUE037371T2 (hu) 2012-12-07 2018-08-28 Vertex Pharma 2-Amino-6-fluor-N-(5-fluor-4-(4-(4-(oxetan-3-il)piperazin-1-karbonil)piperidin-1-il)piridin-3-il) pirazolo[1,5alfa]pirimidin-3-karboxamid mint ATR kináz inhibitor
US8957078B2 (en) 2013-03-15 2015-02-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2016512815A (ja) 2013-03-15 2016-05-09 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Atrキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
EP2970288A1 (de) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Als atr-kinaseinhibitoren nützliche verbindungen
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2014360380B2 (en) 2013-12-06 2019-03-21 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
WO2015092707A2 (en) * 2013-12-17 2015-06-25 Csir A method for identification of anti-hiv human mirna mimics and mirna inhibitors and anti-hiv pharmaceutical compounds
SG11201610197XA (en) 2014-06-05 2017-01-27 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
PL3157566T3 (pl) 2014-06-17 2019-10-31 Vertex Pharma Metoda leczenia nowotworu przy użyciu kombinacji inhibitorów chk1 i atr
WO2016061144A1 (en) 2014-10-14 2016-04-21 The Regents Of The University Of California Use of cdk9 and brd4 inhibitors to inhibit inflammation
JP6854762B2 (ja) 2014-12-23 2021-04-07 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の阻害剤
EP3273966B1 (de) 2015-03-27 2023-05-03 Dana-Farber Cancer Institute, Inc. Hemmer von cyclinabhängigen kinasen
EP3307728A4 (de) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. Kombinationstherapie von transkriptionshemmern und kinasehemmern
JP7028766B2 (ja) 2015-09-09 2022-03-02 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼの阻害剤
WO2017059357A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
RU2633032C1 (ru) * 2016-05-23 2017-10-12 Общество с ограниченной ответственностью "Новые научные технологии" Новые ингибиторы серин-треониновых киназ, в том числе для лечения онкологических заболеваний и туберкулеза
WO2019154177A1 (zh) * 2018-02-12 2019-08-15 恩瑞生物医药科技(上海)有限公司 嘧啶类化合物、其制备方法及其医药用途
MA54092A (fr) 2018-10-30 2021-09-08 Kronos Bio Inc Composés, compositions et procédés de modulation de l'activité de cdk9
CN111393447B (zh) * 2020-05-14 2021-01-15 苏州信诺维医药科技有限公司 一种嘧啶并吡唑类化合物、其制备方法及应用
CN117567460A (zh) * 2022-08-08 2024-02-20 明慧医药(杭州)有限公司 一种前药化合物及其制备方法和用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7119200B2 (en) * 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7605155B2 (en) * 2002-09-04 2009-10-20 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
MY145332A (en) * 2002-09-04 2012-01-31 Schering Corp Trisubstituted 4-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
NZ539165A (en) * 2002-09-04 2008-03-28 Schering Corp Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
CA2624882C (en) * 2005-10-06 2014-05-20 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
EP1942900B1 (de) * 2005-10-06 2015-06-03 Merck Sharp & Dohme Corp. Verwendung von pyrazol-[1,5-a]-pyrimidin-derivaten zur hemmung von proteinkinasen und verfahren zur hemmung von proteinkinasen

Also Published As

Publication number Publication date
IL195238A0 (en) 2009-08-03
AU2007268083A1 (en) 2007-12-06
ZA200809796B (en) 2009-11-25
KR20090019796A (ko) 2009-02-25
PE20080071A1 (es) 2008-02-11
AR061072A1 (es) 2008-07-30
NO20085331L (no) 2009-02-19
EP2027127A1 (de) 2009-02-25
US20070275963A1 (en) 2007-11-29
TW200817404A (en) 2008-04-16
JP2009538304A (ja) 2009-11-05
ECSP088906A (es) 2008-12-30
WO2007139732A1 (en) 2007-12-06
MX2008014824A (es) 2008-12-01
CN101495481A (zh) 2009-07-29
RU2008150419A (ru) 2010-09-20
BRPI0712016A2 (pt) 2011-12-27

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Legal Events

Date Code Title Description
FZDE Discontinued